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AZD4144 | AZD4144 : Inhibitor of NLRP3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NLRP3
    • Ki:14 nM
    • IC50:76 nM
    • IC50:27 nM
    • IC50:25 nM
    Inhibitor
    up to 1 uM

    Selectivity

    Potency
    Cellular
    In Vitro

    NLRP3

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c00781

    In Vivo Validations

    Mouse
    Dose: 0.5 mg/Kg IV, 1 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Plasma half life: 4.0 ± 0.1 IV, 4.0 ± 0.4 PO h
    Systemic clearance: 0.87 ± 0.05 L/h/Kg
    Bioavailability: 53 ± 9%
    Volume of Distribution at Steady-State: 3.0 ± 0.1 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c00781

    Rat
    Dose: 0.5 IV, 1.0 PO mg/Kg
    Route of delivery: Intravenous, Oral
    Plasma half life: 2.9 ± 0.01 IV, 3.0 ± 0.01 h
    Systemic clearance: 0.38 ± 0.02 L/h/Kg
    Bioavailability: 79 ± 6%
    Volume of Distribution at Steady-State: 1.3 ± 0.01 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c00781

    Chemical Information

    Molecular Formula C18H16F3N3O3
    SMILEs OC[C@@H](O)CNc1nnc(-c2ccc(C(F)(F)F)cc2O)c2ccccc12
    InChI InChI=1S/C18H16F3N3O3/c19-18(20,21)10-5-6-14(15(27)7-10)16-12-3-1-2-4-13(12)17(24-23-16)22-8-11(26)9-25/h1-7,11,25-27H,8-9H2,(H,22,24)/t11-/m0/s1
    Molecular weight 379.11 Da
    AlogP 2.7863000000000007
    HBond acceptors 6
    HBond donors 4
    Atoms 43

    References

    Publications

    Cross References

    canSARBindingDB

    Expert Reviews

    by SERP
    (on 4 Dec 2025)
    Cellular Use Rating
    In Model Organisms
    Good cellular and in vivo tool compound for NLRP3. Additional activity data for rats, NLRP subfamily members, and a more general off target panel would be useful.
    by SERP
    (on 18 Dec 2025)
    Cellular Use Rating
    In Model Organisms
    When using the compound in vivo, evaluate several concentrations within the range of 0.3 to 10 mg/kg since it is not possible to determine which dose allowed 50% inhibition based on data plotted in the...
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